Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTGN1ZA)

• DTT Name: Angiotensin II receptor (AGTR)
• Gene Name: AGTR
• DTT Type: Clinical trial target; [1]
• UniProt ID: NOUNIPROTAC
• TTD ID: T85574
• Function: Receptor for angiotensin II. Mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system.
• KEGG Pathway:
  Calcium signaling pathway (hsa04020)
  cGMP-PKG signaling pathway (hsa04022)
  Neuroactive ligand-receptor interaction (hsa04080)
  Adrenergic signaling in cardiomyocytes (hsa04261)
  Vascular smooth muscle contraction (hsa04270)
  Renin-angiotensin system (hsa04614)
  Renin secretion (hsa04924)
  Pathways in cancer (hsa05200)

Molecular Interaction Atlas (MIA) of This DTT

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CYT-006-AngQb	DMIRSWE	Hypertension	BA00-BA04	Phase 2	[1]
DA-727	DM9KS1A	Hypertension	BA00-BA04	Phase 1	[2]

26 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BIBR-363	DMGWFZJ	Hypertension	BA00-BA04	Discontinued in Phase 2	[3]
E-4177	DM2G7IP	Hypertension	BA00-BA04	Discontinued in Phase 2	[4]
Elisartan potassium	DM0XF8J	Hypertension	BA00-BA04	Discontinued in Phase 2	[5]
ETRX-101	DMRB23N	Anemia	3A00-3A9Z	Discontinued in Phase 2	[6]
FK-739	DM7TLF6	Hypertension	BA00-BA04	Discontinued in Phase 2	[7]
ICI-D-8731	DM3R8TX	Hypertension	BA00-BA04	Discontinued in Phase 2	[8]
CGP-48369	DMY8KO4	Hypertension	BA00-BA04	Discontinued in Phase 1	[9]
DuP-532	DM59WQ7	Hypertension	BA00-BA04	Discontinued in Phase 1	[10]
ICI-D-6888	DMZYA9E	Hypertension	BA00-BA04	Discontinued in Phase 1	[11]
A-81282	DMH6LCD	Hypertension	BA00-BA04	Terminated	[12]
A-81988	DM1GLIN	Hypertension	BA00-BA04	Terminated	[13]
BIBS-222	DM5107E	Hypertension	BA00-BA04	Terminated	[14]
BIBS-39	DM098BL	Hypertension	BA00-BA04	Terminated	[14]
BMS-180560	DMWDRI0	Hypertension	BA00-BA04	Terminated	[15]
CI-996	DMCJ7N1	Hypertension	BA00-BA04	Terminated	[16]
DMP-811	DMO26E7	Hypertension	BA00-BA04	Terminated	[17]
EXP-6803	DM9P4ZN	Hypertension	BA00-BA04	Terminated	[18]
FR-149581	DMBOFSQ	Hypertension	BA00-BA04	Terminated	[19]
KW-3433	DMS2KEG	Hypertension	BA00-BA04	Terminated	[20]
L-163017	DMYB5RV	Hypertension	BA00-BA04	Terminated	[21]
ME-3221	DMHX6IC	Hypertension	BA00-BA04	Terminated	[22]
RWJ-46458	DMEO7YD	Hypertension	BA00-BA04	Terminated	[23]
SC-51316	DMB26LO	Hypertension	BA00-BA04	Terminated	[24]
SL-910102	DMNTGXQ	Hypertension	BA00-BA04	Terminated	[25]
WAY-126227	DMTY7PE	Hypertension	BA00-BA04	Terminated	[23]
ZD-7155	DM5KSCI	Hypertension	BA00-BA04	Terminated	[26]

1 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
A-82186	DMQ5AJW	Hypertension	BA00-BA04	Investigative	[27]

References

• [1] CYT-006-AngQb, a vaccine against angiotensin II for the potential treatment of hypertension. Curr Opin Investig Drugs. 2009 Mar;10(3):269-75.
• [2] WO patent application no. 2009,0880,06, Combined pharmaceutical agent.
• [3] Evaluation of the angiotensin challenge methodology for assessing the pharmacodynamic profile of antihypertensive drugs acting on the renin-angiotensin system. Br J Clin Pharmacol. 1999 October; 48(4): 594-604.
• [4] Prevention of renal damage by angiotensin II blockade, accompanied by increased renal hepatocyte growth factor in experimental hypertensive rats. Hypertension. 1999 Aug;34(2):279-84.
• [5] Safety and tolerability of losartan potassium, an angiotensin II receptor antagonist, compared with hydrochlorothiazide, atenolol, felodipine ER, and angiotensin-converting enzyme inhibitors for the treatment of systemic hypertension. Am J Cardiol. 1995 Apr 15;75(12):793-5.
• [6] WO patent application no. 2010,0332,07, Polymer conjugates of therapeutic peptides.
• [7] The pharmacological characterization of FK 739, a new angiotensin II-receptor antagonist. Jpn J Pharmacol. 1993 Nov;63(3):335-43.
• [8] Vasomotor responses in cyclosporin A-treated rats after chronic angiotensin blockade. Hypertension. 1994 Jun;23(6 Pt 2):832-7.
• [9] Antihypertensive therapy augments endothelium-dependent relaxations in coronary arteries of spontaneously hypertensive rats. Circulation. 1994 May;89(5):2212-8.
• [10] DuP 532, an angiotensin II receptor antagonist: first administration and comparison with losartan. Clin Pharmacol Ther. 1997 Jan;61(1):59-69.
• [11] WO patent application no. 1995,0216,09, Treatment of normotensive glaucoma with angiotensin ii antagonists.
• [12] Pharmacological characterization of Abbott-81282, a novel, non-peptide angiotensin-II antagonist selective for type-1 receptors. Life Sci. 1993;53(11):929-37.
• [13] [3H]A-81988, a potent, selective, competitive antagonist radioligand for angiotensin AT1 receptors. Eur J Pharmacol. 1994 Mar 15;267(1):49-54.
• [14] Characterization of BIBS 39 and BIBS 222: two new nonpeptide angiotensin II receptor antagonists. Eur J Pharmacol. 1992 Jul 21;218(1):35-41.
• [15] BMS-180560, an insurmountable inhibitor of angiotensin II-stimulated responses: comparison with losartan and EXP3174. Br J Pharmacol. 1994 Sep;113(1):179-89.
• [16] Pharmacologic characterization of CI-996, a new angiotensin receptor antagonist. J Pharmacol Exp Ther. 1995 Mar;272(3):963-9.
• [17] Disposition of DMP 811 (L-708,404), a potent angiotensin II receptor antagonist, in the rat, monkey, and chimpanzee. Drug Metab Dispos. 1995 Oct;23(10):1104-9.
• [18] Nonpeptide angiotensin II receptor antagonists. IV. EXP6155 and EXP6803. Hypertension. 1989 May;13(5):489-97.
• [19] US patent application no. 2003,0087,306, Methods for identifying novel multimeric agents that modulate receptors.
• [20] Effects of various antihypertensive drugs on the function of osteoblast. Biol Pharm Bull. 2001 Jun;24(6):628-33.
• [21] In vivo pharmacology of an angiotensin AT1 receptor antagonist with balanced affinity for AT2 receptors. Eur J Pharmacol. 1995 Dec 29;294(2-3):439-50.
• [22] Protective effects of ME3221 on hypertensive complications and lifespan in salt-loaded stroke-prone spontaneously hypertensive rats. Clin Exp Pharmacol Physiol. 1996 Mar;23(3):229-35.
• [23] WO patent application no. 1996,0402,58, Spironolactone and angiotensin ii antagonist combination therapy for treatment of congestive heart failure.
• [24] In vitro pharmacology of a nonpeptidic angiotensin II receptor antagonist, SC-51316. J Pharmacol Exp Ther. 1992 Jun;261(3):1037-43.
• [25] A radioreceptor assay for the analysis of AT1-receptor antagonists. Correlation with complementary LC data reveals a potential contribution of active metabolites. J Pharm Biomed Anal. 1998 May;17(1):111-24.
• [26] Comparative cardiovascular effects of the angiotensin II type 1 receptor antagonists ZD 7155 and losartan in the rat. J Pharm Pharmacol. 1996 Aug;48(8):829-33.
• [27] WO patent application no. 2011,0583,31, Pemirolast for the treatment of systemic low grade inflammation.